Indole- and indolizine-glyoxylamides displaying cytotoxicity against multidrug resistant cancer cell lines

Bioorg Med Chem Lett. 2008 Mar 15;18(6):1784-7. doi: 10.1016/j.bmcl.2008.02.029. Epub 2008 Feb 16.

Abstract

We report herein the SAR studies of a series of indole- and indolizine-glyoxylamides that demonstrate substantial in vitro anti-proliferative activities against cancer cell lines, including multidrug resistance (MDR) phenotypes. The in vitro cytotoxic effects have been demonstrated across a wide array of tumor types of various origins (e.g., breast, colon, uterine).

MeSH terms

  • ATP Binding Cassette Transporter, Subfamily B
  • ATP Binding Cassette Transporter, Subfamily B, Member 1 / genetics
  • ATP Binding Cassette Transporter, Subfamily B, Member 1 / metabolism
  • Amides / chemical synthesis
  • Amides / chemistry
  • Amides / pharmacology*
  • Antineoplastic Agents / chemical synthesis
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology*
  • Blotting, Western
  • Cell Death / drug effects
  • Drug Resistance, Multiple*
  • Fluorescent Antibody Technique
  • Humans
  • Indoles / chemistry*
  • Indolizines / chemistry*
  • Neoplasms / drug therapy*
  • RNA, Messenger / genetics
  • RNA, Messenger / metabolism
  • Structure-Activity Relationship
  • Tumor Cells, Cultured

Substances

  • ABCB1 protein, human
  • ATP Binding Cassette Transporter, Subfamily B
  • ATP Binding Cassette Transporter, Subfamily B, Member 1
  • Amides
  • Antineoplastic Agents
  • Indoles
  • Indolizines
  • RNA, Messenger
  • indolizine
  • indole